CA3130237A1 - Formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile - Google Patents

Formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile Download PDF

Info

Publication number
CA3130237A1
CA3130237A1 CA3130237A CA3130237A CA3130237A1 CA 3130237 A1 CA3130237 A1 CA 3130237A1 CA 3130237 A CA3130237 A CA 3130237A CA 3130237 A CA3130237 A CA 3130237A CA 3130237 A1 CA3130237 A1 CA 3130237A1
Authority
CA
Canada
Prior art keywords
compound
formulation
amount
ocular
pain
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CA3130237A
Other languages
English (en)
French (fr)
Inventor
Joseph Paul Bullock
Chinmay Maheshwari
Quintus Medley
Muneto Mogi
Michela MONTECCHI-PALMER
Kalliopi Stasi
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bausch and Lomb Ireland Ltd
Original Assignee
Novartis AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis AG filed Critical Novartis AG
Publication of CA3130237A1 publication Critical patent/CA3130237A1/en
Pending legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40Cyclodextrins; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/14Decongestants or antiallergics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Ophthalmology & Optometry (AREA)
  • Inorganic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Dispersion Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA3130237A 2019-02-15 2020-02-13 Formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile Pending CA3130237A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962806705P 2019-02-15 2019-02-15
US62/806,705 2019-02-15
PCT/IB2020/051211 WO2020165839A1 (en) 2019-02-15 2020-02-13 Formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile

Publications (1)

Publication Number Publication Date
CA3130237A1 true CA3130237A1 (en) 2020-08-20

Family

ID=69740424

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3130237A Pending CA3130237A1 (en) 2019-02-15 2020-02-13 Formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile

Country Status (20)

Country Link
US (3) US11478480B2 (pt)
EP (1) EP3923912A1 (pt)
JP (5) JP6994061B2 (pt)
KR (1) KR20210127197A (pt)
CN (2) CN117752662A (pt)
AU (2) AU2020220957B2 (pt)
BR (1) BR112021015737A2 (pt)
CA (1) CA3130237A1 (pt)
CL (1) CL2021002153A1 (pt)
CO (1) CO2021010689A2 (pt)
CR (1) CR20210428A (pt)
EC (1) ECSP21059628A (pt)
IL (1) IL284628A (pt)
JO (1) JOP20210224A1 (pt)
MX (2) MX2021009704A (pt)
PE (1) PE20212106A1 (pt)
SA (1) SA521430043B1 (pt)
SG (1) SG11202107259QA (pt)
TW (1) TWI827800B (pt)
WO (1) WO2020165839A1 (pt)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6994061B2 (ja) * 2019-02-15 2022-01-14 ノバルティス アーゲー 4-(7-ヒドロキシ-2-イソプロピル-4-オキソ-4h-キナゾリン-3-イル)-ベンゾニトリルの製剤
CA3130038A1 (en) 2019-02-15 2020-08-20 Novartis Ag Methods for treating ocular surface pain
EP4225279A1 (en) * 2020-10-07 2023-08-16 Novartis AG Drug containing dissolvable ocular inserts and method of using same
US20230159202A1 (en) * 2021-11-23 2023-05-25 Bausch + Lomb Ireland Limited Method for making a preservative-free packaged ophthalmic device product
US20240197691A1 (en) * 2022-12-15 2024-06-20 Cn2 Therapeutics, Inc. Tacrolimus compositions and methods of use
CN118340775A (zh) * 2023-01-09 2024-07-16 维眸生物科技(浙江)有限公司 一种含vvn539的眼用组合物及其用途

Family Cites Families (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1280874B (de) 1963-10-09 1968-10-24 Boehringer Sohn Ingelheim 2-Methyl-3-(2-dimethylaminophenyl)-8-amino-3H-chinazolon-(4)
US4027020A (en) 1974-10-29 1977-05-31 Millmaster Onyx Corporation Randomly terminated capped polymers
US3931319A (en) 1974-10-29 1976-01-06 Millmaster Onyx Corporation Capped polymers
US4407791A (en) 1981-09-28 1983-10-04 Alcon Laboratories, Inc. Ophthalmic solutions
US4525346A (en) 1981-09-28 1985-06-25 Alcon Laboratories, Inc. Aqueous antimicrobial ophthalmic solutions
US4836986A (en) 1984-09-28 1989-06-06 Bausch & Lomb Incorporated Disinfecting and preserving systems and methods of use
US5037647A (en) 1988-09-15 1991-08-06 Alcon Laboratories, Inc. Aqueous antimicrobial opthalmic solutions comprised of quaternary ammonium compound, citric acid, citrate and sodium chloride
US5145643A (en) 1990-01-05 1992-09-08 Allergan, Inc. Nonoxidative ophthalmic compositions and methods for preserving and using same
US5300287A (en) 1992-11-04 1994-04-05 Alcon Laboratories, Inc. Polymeric antimicrobials and their use in pharmaceutical compositions
CN1158994C (zh) * 1999-09-24 2004-07-28 爱尔康公司 含环丙沙星和地塞米松的局部悬浮制剂
GB0412769D0 (en) * 2004-06-08 2004-07-07 Novartis Ag Organic compounds
TWI358290B (en) 2004-12-02 2012-02-21 Alcon Inc Topical nepafenac formulations
WO2007056124A2 (en) 2005-11-04 2007-05-18 Hydra Biosciences, Inc. Compounds for modulating trpv3 function
GB0525069D0 (en) 2005-12-08 2006-01-18 Novartis Ag Organic compounds
GB0525068D0 (en) * 2005-12-08 2006-01-18 Novartis Ag Organic compounds
BRPI0620264A2 (pt) 2005-12-22 2011-11-08 Prolexys Pharmaceuticals Inc quinazolonas aril-substituìdas e sua utilização
TW200738232A (en) 2006-01-31 2007-10-16 Alcon Mfg Ltd Use of vanilloid receptor-1 antagonists for the prevention and treatment of glaucoma
EP1964548A1 (en) 2007-03-02 2008-09-03 Novartis AG Pharmaceutical compositions comprising a calcilytic agent
WO2008140750A1 (en) 2007-05-10 2008-11-20 Hydra Biosciences Inc. Compounds for modulating trpv3 function
EP2178562B1 (en) 2007-07-18 2017-08-23 Novartis AG Synergistic combinations of vr-1 antagonists and cox-2 inhibitors
TW200927192A (en) * 2007-11-19 2009-07-01 Alcon Res Ltd Use of TRPV1 receptor antagonists for treating dry eye and ocular pain
WO2009081222A1 (en) 2007-12-21 2009-07-02 Glenmark Pharmaceuticals, S.A. Substituted tricyclic pyridine or pyrimidine vanilloid receptor ligands
WO2009089057A1 (en) 2008-01-09 2009-07-16 Renovis, Ins. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
WO2009090548A2 (en) 2008-01-17 2009-07-23 Glenmark Pharmaceuticals, S.A. 3-azabicyclo [3.1.0] hexane derivatives as vanilloid receptor ligands
US8394779B2 (en) 2008-06-04 2013-03-12 Children's Medical Center Corporation Methods of modulating angiogenesis via TRPV4
WO2010023512A1 (en) 2008-08-28 2010-03-04 Matrix Laboratories Ltd. Novel vanilloid receptor modulators, process for their preparation and pharmaceutical compositions containing them
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
EP2316420B1 (en) 2009-10-22 2014-02-26 Consorzio Universitario Unifarm Topical ophthalmic composition to reduce pain
EP2377850A1 (en) 2010-03-30 2011-10-19 Pharmeste S.r.l. TRPV1 vanilloid receptor antagonists with a bicyclic portion
EP2627178B1 (en) 2010-10-11 2018-05-02 Merck Sharp & Dohme Corp. Quinazolinone-type compounds as crth2 antagonists
CN102659629B (zh) * 2012-02-14 2014-03-19 杭州华东医药集团新药研究院有限公司 化合物及其在制备埃罗替尼中的用途
CN102875480A (zh) 2012-04-23 2013-01-16 中国药科大学 喹唑啉酮类血管抑制剂、其制备方法及其医药用途
GB201215857D0 (en) 2012-09-05 2012-10-24 Sylentis Sau siRNA and their use in methods and compositions for the treatment and/or prevention of eye conditions
MX2015013234A (es) * 2013-03-15 2016-04-15 Inotek Pharmaceuticals Corp Formulaciones oftalmicas.
US20150352176A1 (en) * 2014-06-06 2015-12-10 Newport Research, Inc. Oil-free and fat-free aqueous suspensions of cyclosporin
JP6567648B2 (ja) * 2014-07-28 2019-08-28 サン、ファーマ、アドバンスト、リサーチ、カンパニー、リミテッドSun Pharma Advanced Research Company Limited 薬物のバイオアベイラビリティーの増加および/または眼作用の持続方法
PL3494962T3 (pl) * 2014-09-15 2021-12-06 Verona Pharma Plc Ciekła wziewna kompozycja farmaceutyczna zawierająca RPL554
JP2018507252A (ja) * 2015-01-26 2018-03-15 ボシュ・アンド・ロム・インコーポレイテッドBausch & Lomb Incorporated 眼用懸濁組成物
US11260049B2 (en) 2016-09-20 2022-03-01 Glaxosmithkline Intellectual Property (No. 2) Limited TRPV4 antagonists
JP2019532054A (ja) 2016-09-20 2019-11-07 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited Trpv4拮抗薬
TW201825458A (zh) 2016-09-20 2018-07-16 英商葛蘭素史克智慧財產(第二)有限公司 Trpv4拮抗劑
CA3130038A1 (en) 2019-02-15 2020-08-20 Novartis Ag Methods for treating ocular surface pain
JP6994061B2 (ja) * 2019-02-15 2022-01-14 ノバルティス アーゲー 4-(7-ヒドロキシ-2-イソプロピル-4-オキソ-4h-キナゾリン-3-イル)-ベンゾニトリルの製剤

Also Published As

Publication number Publication date
AU2020220957A1 (en) 2021-08-05
ECSP21059628A (es) 2021-09-30
US11478480B2 (en) 2022-10-25
SA521430043B1 (ar) 2022-11-20
US20200390767A1 (en) 2020-12-17
KR20210127197A (ko) 2021-10-21
MX2021009704A (es) 2021-09-14
BR112021015737A2 (pt) 2021-10-26
JP2022017260A (ja) 2022-01-25
TW202045178A (zh) 2020-12-16
AU2023203933A1 (en) 2023-07-13
US20230139170A1 (en) 2023-05-04
CO2021010689A2 (es) 2021-08-30
US20200261457A1 (en) 2020-08-20
JP2024037806A (ja) 2024-03-19
CN111568906A (zh) 2020-08-25
JOP20210224A1 (ar) 2023-01-30
JP6994061B2 (ja) 2022-01-14
CR20210428A (es) 2021-09-22
SG11202107259QA (en) 2021-08-30
JP2022520795A (ja) 2022-04-01
AU2020220957B2 (en) 2023-04-06
CN117752662A (zh) 2024-03-26
CL2021002153A1 (es) 2022-04-18
CN111568906B (zh) 2023-09-01
TWI827800B (zh) 2024-01-01
JP7465453B2 (ja) 2024-04-11
IL284628A (en) 2021-08-31
MX2024002989A (es) 2024-03-27
WO2020165839A9 (en) 2021-03-18
PE20212106A1 (es) 2021-11-04
JP2020132634A (ja) 2020-08-31
WO2020165839A1 (en) 2020-08-20
EP3923912A1 (en) 2021-12-22
JP2024095674A (ja) 2024-07-10

Similar Documents

Publication Publication Date Title
AU2020220957B2 (en) Formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile
US20240342174A1 (en) Methods for treating ocular surface pain
US20220162170A1 (en) Crystalline forms of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile and formulations thereof
US20230286924A1 (en) Crystalline forms of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile and formulations thereof
JP7571037B2 (ja) 眼表面疼痛を治療する方法

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20240213

EEER Examination request

Effective date: 20240213

EEER Examination request

Effective date: 20240213